Synthesis and antitumor activity evaluation of a novel porphyrin derivative for photodynamic therapy in vitro and in vivo
- 353 Downloads
A novel porphyrin derivative, 5, 10, 15, 20-tetrakis (5-morpholinopentyl)-21H, 23H-Porphin (MPP, 4) and its photophysical characteristics, therapeutic efficacy of photodynamic therapy (PDT) in vitro and in vivo, tumor selectivity, and clearance from normal tissues were investigated here. MPP has strong absorption at relatively long wavelength (λmax = 648 nm, molar absorption coefficient ε ∼ 17,200 M−1cm−1) and can emit strong fluorescence at 653 and 718 nm. When administered to the animal tumor models by tail vein injection, MPP was capable of accumulating in the tumor site, as examined in vivo with the fluorescence signal of MPP. By the combination of MPP and a 650-nm laser irradiation, the viability of T24 cells could decrease by 4.37 %, and inhibition rate of T24 tumor could increase up to 91.21 % compared with control group, demonstrating the potential of MPP as an effective photosensitizer in PDT for tumor treatment.
KeywordsMPP Porphyrin Antitumor Photodynamic therapy Photosensitizer
- MPP 5
10, 15, 20-tetrakis (5-morpholinopentyl)-21H, 23H-Porphin
Reactive oxygen species
Phosphate buffered saline
Cell human bladder cancer cell line
Fetal bovine serum
3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-2H-tetrazolium bromide
This work was supported by Chinese National Natural Science Foundation (No. 21372042, 21402236, 81301878), Foundation of Shanghai government (No.14431906200, 14140903500, 13431900700, 13430722300, 13ZR1441000, 13ZR1440900, 14ZR1439800, 14ZR1439900, 15ZR1439900, 15XD1523400, 14SJGGYY08, 201370), International Cooperation Foundation of China and Croatia (6–11) and Foundation of Yiwu Science and Technology Bureau (No. 2012-G3-02, 2013-G3-03).
Compliance with ethical standards
Conflicts of interest
- 27.Dimitrova DZ, Kubat P, Dimitrov S, Belokonski E, Bogoeva V. Photophysical characterisation and studies of the effect of palladium(II) 5,10,15,20-tetrakis-(4-sulfonatophenyl)-porphyrin on isometric contraction of isolated human mesenteric artery: good news for photodynamic therapy. Photodiagn Photodyn Ther. 2014;11(3):391–9. doi: 10.1016/j.pdpdt.2014.06.002.CrossRefGoogle Scholar